Diprotin A is a tripeptide inhibitor of dipeptidyl peptidase 4 (DPP-4; IC = 1.1 μg/ml). It inhibits degradation of glucagon-like peptide 1 (GLP-1; ) in culture with insulin-secreting BRIN-BD11 rat pancreatic β-cells when used at a concentration of 25 μM. Diprotin A (5 mg/ml) pre-incubation enhances chemotaxis of murine embryonic stem cells towards stromal cell-derived factor-1 (SDF-1/CXCL12) in vitro. Pre-incubation of CD34 human umbilical cord blood cells with diprotin A (5 mM) prior to injection increases engraftment in NOD/SCID recipient mice.
Diprotin A is an inhibitor of dipeptidyl peptidase IV (DPP-IV).
IC50&Target
DPP-4
体外研究
Diprotin A (100 μ M; 30 minutes after treatment with CXCR4 blocker or Src inhibitor) induces phosphorylation of Src [Tyr 416] and VE cadherin [Tyr731] in hEC under normoxic and H/R conditions in human endothelial cells, and disrupts CXCR4 (SDF-1 α receptor) blockade or Src inhibitor to weaken endothelial cell junctions.
Western Blot Analysis
Cell Line:
Human endothelial cells
Concentration:
100 μM
Incubation Time:
30 minutes after CXCR4-blocker or Src-inhibitor treatment
Result:
Induced the phosphorylation of Src [Tyr 416] and VE-cadherin [Tyr731] in hECs.
体内研究
Diprotin A (100 μM; 30 minutes after treatment with CXCR4 blocker or Src inhibitor) induces phosphorylation of Src [Tyr 416] and VE cadherin [Tyr731] in hEC under normoxic and H/R conditions in human endothelial cells, and disrupts CXCR4 (SDF-1 α receptor) blockade or Src inhibitor to weaken endothelial cell junctions.
Animal Model:
Streptozotocin-induced diabetic retinopathy model in wild-type C57/BL6 mice
Dosage:
70 μg/kg
Administration:
Intraperitoneal injection; twice daily; 7 days
Result:
Induced vascular leakage by augmenting the SDF-1α/CXCR4/Src/VE-cadherin signaling pathway.
分子式
C17H31N3O4
分子量
341.45
CAS号
90614-48-5
中文名称
抑二肽素A
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moisture and light, under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month sealed storage, away from moisture and light, under nitrogen)
溶解性数据
In Vitro:
H2O : ≥ 100 mg/mL (292.87 mM)
DMSO : 100 mg/mL (292.87 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
2.9287 mL
14.6434 mL
29.2869 mL
5 mM
0.5857 mL
2.9287 mL
5.8574 mL
10 mM
0.2929 mL
1.4643 mL
2.9287 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。